SML2842
BAY 1125976
≥98% (HPLC)
Synonym(s):
2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide, BAY-1125976, BAY1125976
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About This Item
Empirical Formula (Hill Notation):
C23H21N5O
CAS Number:
Molecular Weight:
383.45
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
BAY 1125976 is an orally active, potent and highly selective AKT1/2 allosteric inhibitor (IC50 = 5.2/18 nM with 10 μM ATP, IC50 = 44/36 nM with 2 mM ATP; AKT3 IC50 = 427 nM with 10 μM ATP) that targets a pocket formed by the kinase & PH domain. BAY 1125976 reduces basal AKT T308/S473 phosphorylation (IC50 = 0.9/1.1; KPL-4 cells) and exhibits anti-cancer efficacy in cultures (IC50 = 0.02-10 μM, 23 human cancer lines) and in xenograft models in vivo (25, 50 mg/kg/day or 5, 15, 25 mg/kg bid. po.; mice), including breast cancers (KPL4 PIK3CAH1074R mutant, MCF7, HBCx-2), AKTE17K-driven prostate cancer LAPC-4, and anal cancer AXF 984.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Oliver Politz et al.
International journal of cancer, 140(2), 449-459 (2016-10-22)
The PI3K-AKT-mTOR signaling cascade is activated in the majority of human cancers, and its activation also plays a key role in resistance to chemo and targeted therapeutics. In particular, in both breast and prostate cancer, increased AKT pathway activity is
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